Tetracyclic anthraquinone antibiotics, in particular doxorubicin and daunorubicin, are widely used anticancer drugs. Doxorubicin has significant curative effects on a lot of solid tumors including liver cancer, gastric cancer, breast cancer, lung cancer, ovary cancer and multiple leukemias. Daunorubicin is one of the most effective drugs for treating leukemia. However, due to their side effects such as sever myelosuppression, cardiac toxicity, adverse reactions of digestive tracts and the like, their clinical applications are restricted. Up to now, a lot of derivatives of tetracyclic anthraquinones have already been separated from nature or prepared artificially. It is intended to find a new generation of anticancer drugs with high activity and low toxicity from these derivatives. The activity in the cellular level of doxorubicin derivative 2-pyrrolinyl-doxorubicin (AN-201) prepared by Attila A. Nagy, et al. is 300-1000 folds of doxorubicin. However, because of the high toxicity of AN-201, the anticancer activity was not observed at the maximal tolerance dose in the pathologic model of transplanted tumor in mice.